Silicon Or Phosphorus Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 540/487)
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Patent number: 9102704Abstract: A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; —CH2—O—C(?O)Me; R8 is OProto, where Proto is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) C(?O)—ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) —CH2—O—C(?O)RC2, where RC2 is methyl or phenyl; (iii) CH2—O—Si—(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) C(—YRC3)(—YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.Type: GrantFiled: October 12, 2012Date of Patent: August 11, 2015Assignee: SPIROGEN SARLInventors: Philip Wilson Howard, Arnaud Tiberghien
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Patent number: 8841257Abstract: Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.Type: GrantFiled: April 9, 2010Date of Patent: September 23, 2014Assignee: Board of Regents, The University of Texas SystemInventors: John S. McMurray, Pijus K. Mandal, Warren S. Liao, Fredika Robertson, Xiaomin Chen, Ramesh Rajaopal, Zhiyong Ren
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Publication number: 20140275522Abstract: A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; —CH2—O—C(?O)Me; R8 is OProto, where Proto is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) C(?O)—ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) —CH2—O—C(?O)RC2, where RC2 is methyl or phenyl; (iii) CH2—O—Si—(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) C(—YRC3)(—YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.Type: ApplicationFiled: October 12, 2012Publication date: September 18, 2014Applicant: SPIROGEN SÁRLInventors: Philip Wilson Howard, Arnaud Tiberghien
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Publication number: 20140087992Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.Type: ApplicationFiled: September 20, 2013Publication date: March 27, 2014Inventors: Ashvinikumar V. Gavai, George V. DeLucca, Daniel O'Malley, Patrice Gill, Claude A. Quesnelle, Brian E. Fink, Yufen Zhao, Francis Y. Lee
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Publication number: 20130137659Abstract: Provided herein are compounds of formula (I):Type: ApplicationFiled: January 25, 2013Publication date: May 30, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130059800Abstract: Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.Type: ApplicationFiled: April 15, 2011Publication date: March 7, 2013Applicants: SEATTLE GENETICS INC., SPIROGEN DEVELOPMENTS SÀRLInventors: Philip Wilson Howard, Luke Masterson, Arnaud Tiberghien, Scott Jeffrey, Patrick Burke, Peter Senter
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Publication number: 20130053347Abstract: The present invention relates to the biology and mechanism of action of the naturally occurring compound Narciclasine, especially as an anti-cancer agent for brain tumors. The invention provides new insights on the target molecule of Amaryllidaceae isocarbostyril derivatives as for example Narciclasine and provides new prodrugs of these Amaryllidceae isocabostyril constituents for treating cancer, specifically cancers or tumors located in the brain.Type: ApplicationFiled: May 3, 2010Publication date: February 28, 2013Applicant: Universite Libre de BruxellesInventors: Veronique Mathieu, Gwendoline Van Goietsenoven, Jacques Dubois, Florence Lefranc-Kiss, Laurent Ingrassia, Robert Kiss
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Patent number: 8378094Abstract: Coupling-initiator compounds are described that include a silicon-containing coupling moiety and at least one polymerization initiator moiety. The coupling moiety may be linked to the at least one polymerization initiator moiety by at least one linking moiety. The coupling moiety is capable of coupling the compound to a substrate, while the one or more polymerization initiator moieties are capable of initiating a polymerization of a monomer under polymerization conditions. The coupling-initiator compounds may be included in fiber reinforced polymer composites, where the compounds are coupled to the fibers in the composites and participate in the polymerization of the surrounding polymer.Type: GrantFiled: March 15, 2010Date of Patent: February 19, 2013Assignee: Johns ManvilleInventors: Kiarash Alavi Shooshtari, Jawed Asrar, Rajappa Tadepalli, Thomas Burghardt, Klaus Friedrich Gleich
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Publication number: 20120097935Abstract: The present invention relates to novel compounds of the formula (I) wherein R1 and R1? independently of each other are H or a substituent, halogen or SiR6R4R5; R2 and R2? may be the same or different and are selected from C1-C25alkyl, C3-C12-cycloalkyl, C2-C25alkenyl, C2-C25alkynyl, C4-C25aryl, C5-C25alkylaryl or C5-C25aralkyl, each of which is unsubstituted or substituted, and under conditions as defined in claim 1, R2 and/or R2? may also be halogen or hydrogen; X is a divalent linking group selected from formula (Ia) and formula (Ib); Y and Y? independently are selected from formula (Ic), formula (Id), formula (Ie), formula (If), formula (Ig); n and p independently range from 0 to 6; where further symbols are as defined in claim 1, and to corresponding oligomers and (co)polymers. The compounds according to the invention are useful as semiconductors and have excellent solubility in organic solvents and excellent film-forming properties.Type: ApplicationFiled: May 21, 2010Publication date: April 26, 2012Applicant: BASF SEInventors: Hans Jürg Kirner, Natalia Chebotareva, Olivier Frédéric Aebischer
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Publication number: 20120035114Abstract: Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.Type: ApplicationFiled: April 9, 2010Publication date: February 9, 2012Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventors: John S. McMurray, Pijus K. Mandal, Warren S. Liao, Fredika Robertson, Xiaomin Chen, Ramesh Rajaopal, Zhiyong Ren
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Publication number: 20120006358Abstract: The invention relates to machine dishwashing agents containing specific polycarbonate-, polyurethane-, and/or polyurea-polyorganosiloxane compounds or precursor compounds thereof of the reactive cyclic carbonate and urea type which help to avoid the formation of water spots and filming after the use of the agents and accelerate the drying of dishes.Type: ApplicationFiled: September 20, 2011Publication date: January 12, 2012Applicant: Henkel AG & Co. KGaAInventors: Nadine Warkotsch, Marc-Steffen Schiedel, Johannes Zipfel, Arnd Kessler
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Patent number: 8080544Abstract: Disclosed are prodrug compounds of formula (I) (wherein variables R1 and R2 are as described herein) which are analogues of an antagonist of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: February 4, 2009Date of Patent: December 20, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Steven N. Gallicchio, Valentino J. Stella
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Publication number: 20110082111Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: December 7, 2010Publication date: April 7, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Sheldon X. Cao, Victoria Feher, Takashi Ichikawa, Benjamin Jones, Stephen W. KALDOR, Andre A. KIRYANOV, Betty Lam, Yan Liu, Christopher McBride, Srinivasa Reddy Natala, Zhe Nie, Jeffrey A. Stafford
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Publication number: 20110062426Abstract: A process for the preparation of a substituted 2,2?-dithiophene is described, which process comprises the steps (a), (c) and optional steps (b) and (d): a reaction of a compound of the formula: with a suitable lithium organic compound, preferably Li-alkyl or Li-alkylamide; b) optional exchange of lithium against another metal selected from Mg1 Zn and Cu; c) reaction of the metallated intermediate obtained in step (a) or (b) with a suitable electrophil, which is CO2 or an aldehyde (addition reaction), or a compound Y?—R17 or Y?—R18-Z (substitution reaction), where R17 and R18 are as defined in claim 1; and optionally d) modification of the product obtained in step (c), e.g. by introducing one or more conjugating moieties Y ring closure between suitable monovalent residues R17, exchange or extension of functional groups or substituents such as addition to carbonyl or substitution of carbonyl in R17 or R18.Type: ApplicationFiled: March 6, 2009Publication date: March 17, 2011Applicant: BASF SEInventors: Hans Jurg Kirner, Frank Bienewald, Jean Charles Flores, Oliver Frédéric Aebischer
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Publication number: 20100298269Abstract: Disclosed are prodrug compounds of formula (I) (wherein variables R1 and R2 are as described herein) which are analogues of an antagonist of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: February 4, 2009Publication date: November 25, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Steven N. Gallicchio, Valentino J. Stella
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Publication number: 20100280239Abstract: Coupling-initiator compounds are described that include a silicon-containing coupling moiety and at least one polymerization initiator moiety. The coupling moiety may be linked to the at least one polymerization initiator moiety by at least one linking moiety. The coupling moiety is capable of coupling the compound to a substrate, while the one or more polymerization initiator moieties are capable of initiating a polymerization of a monomer under polymerization conditions. The coupling-initiator compounds may be included in fiber reinforced polymer composites, where the compounds are coupled to the fibers in the composites and participate in the polymerization of the surrounding polymer.Type: ApplicationFiled: March 15, 2010Publication date: November 4, 2010Inventors: Kiarash Alavi Shooshtari, Jawed Asrar, Rajappa Tadepalli, Thomas Burghardt, Klaus Friedrich Gleich
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Publication number: 20090005528Abstract: In one aspect, the invention relates to silicon-based prepolymers. The disclosed prepolymers exhibit satisfactory solubility in aqueous solutions or hydrophilic solutions and can overcome undesirable shrinkage, expansion, and related problems possessed by conventional silicone monomers and related conventional polymerization techniques by producing hydrogels from a crosslinkable prepolymer. Also disclosed are polymers and molded articles produced from the disclosed prepolymers, which attain a satisfactory oxygen permeability. Also disclosed are methods for producing the disclosed prepolymers. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 29, 2007Publication date: January 1, 2009Inventors: Kazuhiko Fujisawa, Mitsuru Yokota, Masataka Nakamura
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Publication number: 20080318905Abstract: Prodrugs of parent drugs and methods of making and using the same are described. The prodrugs comprise an amine-containing parent drug moiety and a prodrug moiety, such as methoxyphosphonic acid or ethoxyphosphonic acid. The prodrugs may be employed in therapy for the treatment of various indications, such as pain, and in methods of decreasing the abuse potential of abuse-prone drugs and/or delaying the onset of parent drug activity and/or prolonging parent drug activity as compared to administration of a parent drug.Type: ApplicationFiled: December 5, 2007Publication date: December 25, 2008Inventors: Naweed Muhammad, Keith R. Bley
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Patent number: 7368444Abstract: The present invention relates to the compound presented by formula (I) (wherein all symbols in formula (I) are the same mean as the description shown in the specification.), mitocondorial benzogeazepin receptor (MBR) antagonist comprising the compound, the preventive and/or treatment medicine against diseases caused by stress of which an active ingredient is the compound. Since the compound represented by formula (I) has MBR antagonistic activity, and controls the production of neurosteroid, it is useful as the preventive and/or treatment medicine against diseases caused by stress.Type: GrantFiled: February 13, 2003Date of Patent: May 6, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Seishi Katsumata, Masashi Kato, Jun-ichiro Manako, Kazuyuki Ohmoto
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Patent number: 6686350Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: January 25, 1999Date of Patent: February 3, 2004Assignee: Biogen, Inc.Inventors: Zhongli Zheng, Carol L. Ensinger, Steven P. Adams
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Publication number: 20030176398Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.Type: ApplicationFiled: June 11, 2002Publication date: September 18, 2003Inventors: Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fayang G. Qiu, Fenmei Yao, Jia-Ning Xiang, Ian R. Ollmann
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Publication number: 20030149262Abstract: The present invention describes novel compounds of the formula:Type: ApplicationFiled: November 26, 2002Publication date: August 7, 2003Inventors: Edward H. Cheesman, Michael Sworin
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Publication number: 20030139377Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections: 1Type: ApplicationFiled: November 12, 2002Publication date: July 24, 2003Applicant: SmithKline Beecham CorporationInventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld
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Publication number: 20030134827Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1Type: ApplicationFiled: March 12, 2002Publication date: July 17, 2003Inventors: Jingwu Duan, Carl P. Decicco, Zelda R. Wasserman, Thomas P. Maduskuie
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Patent number: 6576760Abstract: Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the polyamines except two being fully substituted and the remaining two bearing one H atom each, are cyclized by reaction with a bridging agent that contains two sites that each bear a reactive group capable of undergoing a nucleophilic attack by one of the two N-H groups on the polyamine. Unlike the prior art, cyclization occurs in preference over polymerization of the polyamine, even in reaction mixtures in which the polyamine is at high concentration. A process is also disclosed whereby linear polyamines in which the terminal amine groups are primary amines are substituted with methylenephosphonate ester groups, with one such substituent on each nitrogen atom of the polyamine.Type: GrantFiled: January 11, 2001Date of Patent: June 10, 2003Assignee: Chelator LLCInventors: Harry S. Winchell, Rosa L. Cyjon, Joseph Y. Klein, Elliot D. Simhon, Ofer Klein, Haim Zaklad
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Publication number: 20030092677Abstract: The present invention is a compound of formula 1Type: ApplicationFiled: November 20, 2002Publication date: May 15, 2003Inventors: Geo Adam, Alaxander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
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Patent number: 6521613Abstract: Compounds, compositions and methods are disclosed useful for enhancing penetration of a pharmacologically active substances across skin or tissue membranes. Compounds for use in such compositions and methods are highly water-soluble N-substituted polyalkylene oxide derivatives of cyclic amides. A compound of the invention has the structural formula: wherein m is an integer from 2 to about 6, n is an integer from 1 to about 8, and R is hydrogen, trimethylsilyl or lower alkyl.Type: GrantFiled: April 10, 2001Date of Patent: February 18, 2003Assignee: Allergan, Inc.Inventor: Gary Ewing
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Patent number: 6503898Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.Type: GrantFiled: July 10, 1998Date of Patent: January 7, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Yuk-Sun Lam, Prabhakar Kondaji Jadhav, Charles Joseph Eyermann, Carl Nicholas Hodge, George Vincent De Lucca, James David Rodgers
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Patent number: 6399598Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptacle salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: March 1, 2000Date of Patent: June 4, 2002Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
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Patent number: 6372735Abstract: Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereof. The compounds are useful as antiallergic agents and exhibit excellent bioavailability.Type: GrantFiled: March 29, 2000Date of Patent: April 16, 2002Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yasuo Ohtsuka, Toshio Nishizuka, Sohjiro Shiokawa, Seiji Tsutsumi, Mami Kawaguchi, Hideo Kitagawa, Hiromi Takata, Takashi Shishikura, Toyoaki Ishikura, Kenichi Fushihara, Yumiko Okada, Sachiko Miyamoto, Maki Shiobara
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Publication number: 20020042398Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1Type: ApplicationFiled: July 10, 2001Publication date: April 11, 2002Inventors: Thomas P. Maduskuie, Jingwu Duan, Stephen E. Mercer
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Publication number: 20020042508Abstract: The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.Type: ApplicationFiled: September 20, 2001Publication date: April 11, 2002Inventors: Neil Warren Boaz, Sheryl Davis Debenham
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Patent number: 6344560Abstract: A nitroaromatic compound is used to enhance the solubility of a nitroxyl compound in an aromatic hydrocarbon solvent.Type: GrantFiled: May 3, 2000Date of Patent: February 5, 2002Assignee: Uniroyal Chemical Company, Inc.Inventors: Brendan J. Geelan, Brigitte Benage, Gerald J. Abruscato, Kirk A. Schlup, Ruben S. Grewal, Andrew J. Eisenstein
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Publication number: 20020004494Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: May 22, 2001Publication date: January 10, 2002Inventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
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Patent number: 6323195Abstract: This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12alkylcarbonyl, (C1-C12)alkoxycarbonyl, mono(C1-C12)alkylaminocarbonyl, or di(C1-C12)alkylaminocarbonyl; R2 is hydrogen, (C3-C12)alkenylcarbonyloxy, (C3-C12)cycloalkylcarbonyloxy, (C3-C12)cycloalkyl(C1-C12)alkylcarbonyloxy, oxygen containing heterocycloxy, oxygen containing heterocyclylcarbonyloxy, sulfur containing heterocyclyloxy, sulfur containing heterocyclylcarbonyloxy, nitrogen containing hetercyclyloxy, nitrogen containing heterocyclylcarbonyloxy, haloalkylsulfonyloxy, (C1-C6)alkylsilyloxy; R3 is hydrogen, halo or (C1-C4)alkyl; R4 is hydrogen or (C1-C6)alkyl; with the proviso that R1 and R2 are not both hydrogen when R3 and R4 are hydrogen; all geometric, and optical stereoisomers thereof, or a pharmaceutically acceptable addition salt thereof; which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing tType: GrantFiled: October 15, 1993Date of Patent: November 27, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
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Patent number: 6262222Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.Type: GrantFiled: October 8, 1998Date of Patent: July 17, 2001Assignee: Hyundai Electronics Industries Co., Ltd.Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
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Patent number: 6207663Abstract: Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: October 5, 1999Date of Patent: March 27, 2001Assignees: Hoechst Atkiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel LeFrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 6130231Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: November 26, 1997Date of Patent: October 10, 2000Assignee: DuPont PharmaceuticalsInventors: John Wityak, Aleksandra Ewa Tobin
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Patent number: 6121258Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: August 26, 1997Date of Patent: September 19, 2000Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
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Patent number: 6114522Abstract: A process for producing 4-substituted-3-halogeno-1,4-benzoxazepin derivative or the salt thereof comprising: deprotonizing a benzoxazepine derivative having the formula (II): ##STR1## with a base; and then, reacting the deprotonized product with a phosphate halide to produce an intermediate having the formula (IV): ##STR2## and then, reacting the resultant intermediate (IV) with a reagent selected from (i) a complex of a phosphine with chlorine or bromine, (ii) a phosphine and a chlorine gas or liquid bromine, (iii) a phosphine and tetrachloromethane or tetrabromomethane, or (iv) a halogenated phosphite ester to produce a 4-substituted-3-halogeno-1,4-benzoxazepine derivative having the formula (I) ##STR3## wherein X indicates a chlorine atom or a bromine atom, or its salt.Type: GrantFiled: November 24, 1999Date of Patent: September 5, 2000Assignee: Suntory LimitedInventors: Kastuhide Kamei, Noriko Maeda, Toshio Tatsuoka
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Patent number: 6051678Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.Type: GrantFiled: March 13, 1997Date of Patent: April 18, 2000Assignee: Hyundai Electronics Industries Co., Ltd.Inventors: Jin Baek Kim, Min Ho Jung, Jong Ho Cheong
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Patent number: 6034215Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: October 14, 1997Date of Patent: March 7, 2000Assignee: Corvas International, Inc.Inventors: Joseph Edward Semple, Robert John Ardecky, Ruth Foelsche Nutt, William Charles Ripka, David C. Rowley, Marguerita S. L. Lim-Wilby, Terence Kevin Brunck
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Patent number: 5994537Abstract: Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.Type: GrantFiled: February 14, 1998Date of Patent: November 30, 1999Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5981511Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: March 5, 1997Date of Patent: November 9, 1999Assignee: G.D. Searle & Co.Inventors: Rolando E. Gapud, Timothy J. Hagen, Ann E. Hallinan, Donald W. Hansen, Jr., Robert E. Manning, Suzanne Metz, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, R. Keith Webber
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Patent number: 5955606Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.Type: GrantFiled: February 19, 1998Date of Patent: September 21, 1999Assignee: Hyundai Electronics Industries Co., Ltd.Inventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
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Patent number: 5952327Abstract: Compounds having NEP-inhibitory activity, corresponding to the formula I in whichR.sup.1 is hydrogen or a group forming a biolabile phosphonic acid ester,R.sup.2 is hydrogen or a group forming a biolabile phosphonic acid ester andR.sup.3 is hydrogen or a group forming a biolabile carboxylic acid esterand physiologically acceptable salts of acids of formula I, and pharmaceutical compositions comprising these compounds.Type: GrantFiled: November 12, 1998Date of Patent: September 14, 1999Assignee: Solvay Pharmaceuticals GmbHInventors: Harald Waldeck, Joerg Meil, Dirk Thormaehlen, Michael Wurl
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Patent number: 5952462Abstract: Antigens capable of eliciting antibodies which can catalyze chemical reactions, in particular, the cleavage or formation of a peptide linkage, comprising a hapten or a hapten and a suitable carrier molecule are disclosed. Haptens include, among others, silicon and boron containing compounds. Antibodies which are catalytically active for chemical reactions, in particular, the cleavage or formation of a selected peptide linkage or an ester bond, and which are elicited by such antigens are disclosed as well as methods for producing the antibodies and methods for catalyzing the cleavage or formation of a peptide linkage or in ester bond in a molecule.Type: GrantFiled: November 2, 1994Date of Patent: September 14, 1999Assignee: IGEN International Inc.Inventors: Michael J. Powell, Richard C. Titmas, Richard J. Massey
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Patent number: 5945408Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: August 8, 1996Date of Patent: August 31, 1999Assignee: G.D. Searle & Co.Inventors: R. Keith Webber, Foe S. Tjoeng, Robert E. Manning
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Patent number: 5942638Abstract: A synthetic process for the selective preparation of reactive polyhedral oligomeric silsesquioxanes (POSS) as well as polyhedral oligomeric silicate (POS) (spherosilicate) is provided. The method claimed herein employs metal catalyzed metathesis reactions for the selective reaction of .alpha.-olefin containing polyhedral oligomeric silsesquioxanes or silicates with olefinic reagents bearing functionalities useful for grafting reactions, polymerization chemistry and sol-gel processes. The use of metal catalyzed metathesis chemistry to form both linear or network polyhedral silsesquioxane polymers directly from .alpha.-olefin-containing polyhedral oligomeric silsesquioxanes is also described.Type: GrantFiled: January 5, 1998Date of Patent: August 24, 1999Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Joseph D. Lichtenhan, Joseph J. Schwabb, Frank J. Feher, Daravong Soulivong
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Patent number: 5939576Abstract: A synthetic process for the selective preparation of reactive polyhedral oligomeric silsesquioxanes (POSS) as well as polyhedral oligomeric silicate (POS) (spherosilicate) is provided. The inventive process employs the use of metal catalyzed hydrosilylation reactions for the selective reaction of silane containing polyhedral oligomeric silsesquioxanes or silicates with olefinic reagents bearing functionalities useful for grafting reactions, polymerization chemistry and sol-gel processes. The invention also discloses metal-catalyzed hydrosulfidation reactions and metal-catalyzed hydrophosphidation reacttions for functionalization of polycyclic silicones.Type: GrantFiled: January 5, 1998Date of Patent: August 17, 1999Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Joseph D. Lichtenhan, Joseph J. Schwab, Frank J. Feher, Daravong Soulivong